Synthesis and in vitro antitubercular evaluation of novel sansanmycin derivatives

Tuberculosis (TB) is a major health problem worldwide. A series of novel sansanmycin derivatives were designed, semi-synthesized and evaluated for their activity against drug-susceptible Mycobacterium tuberculosis strain H 37Rv with sansanmycin A (SSA) as the lead. Among these analogs tested, compou...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2011-11, Vol.21 (22), p.6804-6807
Main Authors: Li, Yang-Biao, Xie, Yun-Ying, Du, Na-Na, Lu, Yu, Xu, Hong-Zhang, Wang, Bin, Yu, Ying, Liu, Yan-Xin, Song, Dan-Qing, Chen, Ru-Xian
Format: Article
Language:English
Subjects:
Antibacterial agents
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antitubercular
Antitubercular Agents - chemical synthesis
Antitubercular Agents - chemistry
Antitubercular Agents - pharmacology
Biological and medical sciences
China
Drug-resistance
Humans
Medical sciences
Microbial Sensitivity Tests
Mycobacterium tuberculosis
Mycobacterium tuberculosis - drug effects
Oligopeptides - chemical synthesis
Oligopeptides - chemistry
Oligopeptides - pharmacology
Pharmacology. Drug treatments
Sansanmycin
Streptomyces - chemistry
Structure–activity relationship
Tuberculosis - drug therapy
Tuberculosis, Multidrug-Resistant
Uridine - analogs & derivatives
Uridine - chemical synthesis
Uridine - chemistry
Uridine - pharmacology
Uridyl peptide
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Summary:Tuberculosis (TB) is a major health problem worldwide. A series of novel sansanmycin derivatives were designed, semi-synthesized and evaluated for their activity against drug-susceptible Mycobacterium tuberculosis strain H 37Rv with sansanmycin A (SSA) as the lead. Among these analogs tested, compound 1d possessing an isopropyl group at the amino terminal afforded an increased antimycobacterial activity with a MIC value of 8 μg/mL in comparison with SSA. Importantly, it was active for rifampicin- and isoniazid-resistant M. tuberculosis strain isolated from patients in China. These promising results offer an opportunity for further exploration of this novel class of analogs as antitubercular agents.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2011.09.031